New pyrazoles and pyrazolo[3,4-b] pyridines were synthesized and their structure was confirmed by elemental analyses as well as IR, H NMR, C NMR, and mass spectral data. All the newly synthesized derivatives were evaluated in vitro for inhibitory activity against COX-1 and COX-2 enzymes and their IC values were calculated, most of the derivatives showed good inhibitory activity with derivatives IVb, IVh and IVJ showing inhibitory activity better than celecoxib. Moreover, the eight most potent derivatives IVa, IVb, IVc, IVd, IVe, IVh, IVJ, and IVL were selected for in vivo assay to measure their effect on paw edema in rates and their ulcerogenic effect. Compounds IVa, IVb and IVc were found to be the most active and selective as COX-2 inhibitors and most effective in protection from edema, they were also found to have lowest ulcerogenic effect among all derivatives.
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http://dx.doi.org/10.1016/j.bioorg.2018.10.014 | DOI Listing |
Phytother Res
January 2025
College of Veterinary Medicine, Yangzhou University, Yangzhou, China.
The rising prevalence of multidrug-resistant (MDR) Gram-positive bacteria threatens the effectiveness of current antibiotic therapies. However, the development of new antibiotics has stagnated in recent years, highlighted the critical need for the discovery of innovative antimicrobial agents. This study aims to evaluate the antibacterial activity of naphthoquinones derived from Arnebia euchroma (Royle) Johnst (ADNs) and elucidate their underlying mechanisms.
View Article and Find Full Text PDFFront Pharmacol
December 2024
Department of Biosciences, Integral University, Lucknow, India.
Introduction: Diabetic retinopathy is a significant microvascular disorder and the leading cause of vision impairment in working-age individuals. Hyperglycemia triggers retinal damage through mechanisms such as the polyol pathway and the accumulation of advanced glycation end products (AGEs). Inhibiting key enzymes in this pathway, aldose reductase (AR) and sorbitol dehydrogenase (SD), alongside preventing AGE formation, may offer therapeutic strategies for diabetic retinopathy and other vascular complications.
View Article and Find Full Text PDFMediators Inflamm
December 2024
Biomedical Research Center, Slovak Academy of Sciences, Bratislava, Slovakia.
Spontaneous tumor regression is a recognized phenomenon across various cancer types. Recent research emphasizes the alterations in autoantibodies against carbonic anhydrase I (CA I) (anti-CA I) levels as potential prognostic markers for various malignancies. Particularly, autoantibodies targeting CA I and II appear to induce cellular damage by inhibiting their respective protein's catalytic functions.
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December 2024
Institute of Reconstructive Neurobiology, Medical Faculty and University Hospital of Bonn, University of Bonn, Bonn, Germany.
Brain aging is a chronic process linked to inflammation, microglial activation, and oxidative damage, which can ultimately lead to neuronal loss. Sialic acid-binding immunoglobulin-like lectin-11 (SIGLEC-11) is a human lineage-specific microglial cell surface receptor that recognizes -2-8-linked oligo-/polysialylated glycomolecules with inhibitory effects on the microglial inflammatory pathways. Recently, the gene locus was prioritized as a top tier microglial gene with potential causality to Alzheimer's disease, although its role in inflammation and neurodegeneration remains poorly understood.
View Article and Find Full Text PDFFront Plant Sci
December 2024
Institute of Bast Fiber Crops, Chinese Academy of Agricultural Sciences, Changsha, China.
Bacterial canker is a devastating disease in kiwifruit production, primarily caused by pv. . In this study, a strain of named JIN4, isolated from a kiwifruit branch, showed antagonistic activity.
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